Halopemide and benzodiazepine binding sites.

Halopemide inhibits 3H-BZ binding to crude and washed rat forebrain membranes with IC50 values of 16-25 microM. Its putative metabolites are considerably less active. The actions of halopemide are probably not directly related to its ability to interfere with high-affinity 3H-GABA binding sites. However, halopemide may have some unique properties in this regard.